Tuesday, 24 May 2005 - 2:35 PM
635

This presentation is part of: Proteinase

Medicinal Chemistry and Properties of 1,2,4-Thiadiazoles

Tim Fat Tam, Regis Leung-Toung, Warren Li, Michael Spino, and Khashayar Karimain. ApoPharma Inc., Toronto, ON, Canada

1,2,4-Thiadiazole is a distinctive class of small heterocyclic thiol trapping agents that serve as an interesting pharmacophore in the design of inhibitors targeting the cysteine residues of proteins. X-Ray crystal structures of enzyme-inhibitor complex indicate that the cysteine thiol reacts with the N-S bond of the thiadiazole moiety to form a disulfide bond resulting in the inactivation of the enzymes. This presentation addresses the medicinal chemistry and various properties of 1,2,4-thiadiazoles in their potential as new electrophilic “warheads” for targeting the cysteine residues of biomolecules (e.g, H+/K+ ATPase), and cysteine-dependent enzymes (e.g., cathepsin B and transglutaminase).

Keywords: Thiadiazole, proton pump, cathepsin B, Factor XIIIa, transglutaminase, cysteine thiol, inhibitors


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